PE20161386A1 - AZOL AMIDO-SUBSTITUTED COMPOUNDS AS INHIBITORS OF TNKS1 AND / OR TNKS2 - Google Patents

AZOL AMIDO-SUBSTITUTED COMPOUNDS AS INHIBITORS OF TNKS1 AND / OR TNKS2

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Publication number
PE20161386A1
PE20161386A1 PE2016001850A PE2016001850A PE20161386A1 PE 20161386 A1 PE20161386 A1 PE 20161386A1 PE 2016001850 A PE2016001850 A PE 2016001850A PE 2016001850 A PE2016001850 A PE 2016001850A PE 20161386 A1 PE20161386 A1 PE 20161386A1
Authority
PE
Peru
Prior art keywords
alkyl
tnks1
tnks2
inhibitors
azol
Prior art date
Application number
PE2016001850A
Other languages
Spanish (es)
Inventor
Jozsef Balint
Knut Eis
Michaela Bairlein
Simon Holton
Detlev Sulzle
Marcus Bauser
Franziska Siegel
Ningshu Liu
Philip Lienau
Volkhart Min-Jian Li
Eckhard Bender
Stefan Golz
Daniel Basting
Sarah Wagner
Jens Ackerstaff
Philipp Buchgraber
Original Assignee
Bayer Pharma AG
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Filing date
Publication date
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20161386A1 publication Critical patent/PE20161386A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/092—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
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    • C07D491/10—Spiro-condensed systems
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Abstract

La presente invencion se refiere a derivados de azol sustituidos con amida de formula (I), donde: X1 es NR3 u O; X2 es CR6 o N; R1 es -OR9 o -N(R10)R11; R2 es H, C1-C3-alquilo y C3-C4-cicloalquilo; R3 R4 y R7 son H; R5 es H, C1-C3-alquilo, C1-C3-alcoxilo, entre otros; R6 es H o halogeno; R8 es arilo o heteroarilo opcionalmente sustituidos; R9 es C1-C6-alquilo, C3-C6-cicloalquilo, entre otros; R10 Y R11 son H, C1-C6-alquilo, entre otros o R10 y R11 junto con N forman un grupo heterocicloalquilo de 4 a 6 miembros opcionalmente sustituido o R10 y R11 junto con N forman a), b), entre otros, donde * es el punto de union con el resto de la molecula. Son preferidos: N5-{4-[(2,3-diclorobenzoil)amino]fenil}-N4-metil-1H-imidazol-4,5-dicarboxamida; N5-(4-{[(2-cloropiridin-3-il) carbonil]amino}fenil)-N4-metil-1H-imidazol-4,5-dicarboxamida, entre otros. Tambien se refiere a un metodo de preparacion, una composicion farmaceutica y una combinacion. Dichos compuestos son inhibidores de la Tankirasa 1 (TNKS1) y/o Tankirasa 2 (TNKS2) siendo utiles en el tratamiento de enfermedades, como cancer, envejecimiento, enfermedades metabolicas, entre otrosThe present invention relates to amide-substituted azole derivatives of formula (I), where: X1 is NR3 or O; X2 is CR6 or N; R1 is -OR9 or -N (R10) R11; R2 is H, C1-C3-alkyl and C3-C4-cycloalkyl; R3 R4 and R7 are H; R5 is H, C1-C3-alkyl, C1-C3-alkoxy, among others; R6 is H or halogen; R8 is optionally substituted aryl or heteroaryl; R9 is C1-C6-alkyl, C3-C6-cycloalkyl, among others; R10 AND R11 are H, C1-C6-alkyl, among others or R10 and R11 together with N form an optionally substituted 4- to 6-membered heterocycloalkyl group or R10 and R11 together with N form a), b), among others, where * is the point of union with the rest of the molecule. Preferred are: N5- {4 - [(2,3-dichlorobenzoyl) amino] phenyl} -N4-methyl-1H-imidazole-4,5-dicarboxamide; N5- (4 - {[(2-chloropyridin-3-yl) carbonyl] amino} phenyl) -N4-methyl-1H-imidazole-4,5-dicarboxamide, among others. It also refers to a method of preparation, a pharmaceutical composition and a combination. Said compounds are inhibitors of Tankirase 1 (TNKS1) and / or Tankirase 2 (TNKS2), being useful in the treatment of diseases, such as cancer, aging, metabolic diseases, among others.

PE2016001850A 2014-04-02 2015-04-01 AZOL AMIDO-SUBSTITUTED COMPOUNDS AS INHIBITORS OF TNKS1 AND / OR TNKS2 PE20161386A1 (en)

Applications Claiming Priority (2)

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Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017055313A1 (en) 2015-10-01 2017-04-06 Bayer Pharma Aktiengesellschaft Amido-substituted azole compounds
WO2017055316A1 (en) 2015-10-01 2017-04-06 Bayer Pharma Aktiengesellschaft Amido-substituted azole compounds
TWI808055B (en) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Combination therapies of hdac inhibitors and pd-1 inhibitors
TWI794171B (en) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Combination therapies of hdac inhibitors and pd-l1 inhibitors
WO2018078009A1 (en) 2016-10-29 2018-05-03 Bayer Pharma Aktiengesellschaft Amido-substituted cyclohexane derivatives
WO2018078005A1 (en) 2016-10-29 2018-05-03 Bayer Pharma Aktiengesellschaft Amido-substituted azaspiro derivatives as tankyrase inhibitors
WO2018087126A1 (en) 2016-11-09 2018-05-17 Bayer Pharma Aktiengesellschaft Amido-substituted cyclohexane derivatives as inhibitors of tankyrase

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5616489A (en) 1979-07-20 1981-02-17 Ajinomoto Co Inc Imidazolecarboxylic acid derivative
DE60032483T2 (en) 1999-06-24 2007-04-19 Nihon Nohyaku Co., Ltd. DIAMIDE DERIVATIVES OF HETEROCYCLIC DICARBOXYLIC ACIDS, INSECTICIDES FOR ACORM AND GARDENING AND A METHOD OF USE THEREOF
DE102004058062A1 (en) 2004-12-02 2006-06-08 Bayer Healthcare Ag Cyclic iminocarbamates and their use
US7562189B2 (en) 2006-09-28 2009-07-14 Network Appliance, Inc. Write-in-place within a write-anywhere filesystem
CA2663856A1 (en) 2006-09-28 2008-04-10 Exelixis, Inc. Jak-2 modulators and methods of use
EP2217223A2 (en) 2007-11-05 2010-08-18 Novartis AG Methods and compositions for measuring wnt activation and for treating wnt-related cancers
US8440710B2 (en) 2009-10-15 2013-05-14 Hoffmann-La Roche Inc. HSL inhibitors useful in the treatment of diabetes
US9725479B2 (en) 2010-04-22 2017-08-08 Ionis Pharmaceuticals, Inc. 5′-end derivatives
US9096587B2 (en) 2010-12-08 2015-08-04 Oslo University Hospital Hf Triazole derivatives as Wnt signaling pathway inhibitors
US8722721B2 (en) 2011-03-16 2014-05-13 Hoffmann-La Roche Inc. SEC-hydroxycyclohexyl derivatives
WO2013012723A1 (en) 2011-07-13 2013-01-24 Novartis Ag Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors
US9227982B2 (en) 2011-07-13 2016-01-05 Novartis Ag 4-oxo-3,5,7,8-tetrahydro-4H-pyrano[4,3-d]pyrminidinyl compounds for use as tankyrase inhibitors
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
AR088218A1 (en) 2011-07-19 2014-05-21 Infinity Pharmaceuticals Inc USEFUL HETEROCICLICAL COMPOUNDS AS PI3K INHIBITORS
EP2751093A1 (en) 2011-08-29 2014-07-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2013093508A2 (en) * 2011-12-22 2013-06-27 Oslo University Hospital Hf Wnt pathway inhibitors
WO2013134079A1 (en) 2012-03-05 2013-09-12 Amgen Inc. Oxazolidinone compounds and derivatives thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
HUE028325T2 (en) 2012-05-04 2016-12-28 Merck Patent Gmbh Pyrrolotriazinone derivatives
WO2013177349A2 (en) 2012-05-25 2013-11-28 Glaxosmithkline Llc Quinazolinediones as tankyrase inhibitors
WO2013182546A1 (en) 2012-06-07 2013-12-12 F. Hoffmann-La Roche Ag Pyrazolopyrimidone and pyrazolopyridone inhibitors of tankyrase
CN104395314A (en) 2012-06-20 2015-03-04 霍夫曼-拉罗奇有限公司 Pyrrolopyrazone inhibitors of tankyrase
UA110310C2 (en) 2012-06-20 2015-12-10 Ф. Хоффманн-Ля Рош Аг Compounds n-aryl triazole as antagonists receptors lisophosphatidic acid (lpar)
LT2882714T (en) 2012-08-08 2020-03-10 Merck Patent Gmbh (aza-)isoquinolinone derivatives
JP6497520B2 (en) 2013-05-23 2019-04-10 日産化学株式会社 Liquid crystal aligning agent, liquid crystal alignment film, and liquid crystal display element
CN103923237B (en) 2013-10-31 2017-01-25 北京利和知信科技有限公司 Catalyst component for olefin polymerization and application thereof
KR101916701B1 (en) 2014-09-26 2018-11-08 창저우 인셩 파마슈티칼 캄파니 리미티드 Benzofuran analogue as ns4b inhibitor
PE20181024A1 (en) 2015-05-05 2018-06-27 Bayer Pharma AG DERIVATIVES OF CYCLOHEXANE SUBSTITUTED WITH AMIDO
WO2017055313A1 (en) 2015-10-01 2017-04-06 Bayer Pharma Aktiengesellschaft Amido-substituted azole compounds
WO2017055316A1 (en) 2015-10-01 2017-04-06 Bayer Pharma Aktiengesellschaft Amido-substituted azole compounds

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